ROR gamma-t-IN-1 Chemical Properties

Boiling point:

617.1±55.0 °C(Predicted)

Density 

1.434±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMF:3.0(Max Conc. mg/mL);5.64(Max Conc. mM)
DMSO:68.33(Max Conc. mg/mL);128.36(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:2):0.3(Max Conc. mg/mL);0.56(Max Conc. mM)
Ethanol:50.0(Max Conc. mg/mL);93.92(Max Conc. mM)

form 

A crystalline solid

pka

12.33±0.70(Predicted)

ROR gamma-t-IN-1 Usage And Synthesis

Description

GSK805 is a potent, orally bioavailable retinoid-related orphan receptor gamma t (RORγt) inverse agonist that interacts with the receptor''s putative ligand binding domain without exerting significant effects on DNA binding. It inhibits the expression of IL-17 (at 0.5 μM) in naïve CD4⁺ T cells activated under Th17-cell-polarizing conditions and affects the broader RORγt-dependent gene network, inhibiting the development and pathogenic function of Th17 cells. GSK805 significantly reduces the severity of experimental autoimmune encephalomyelitis (EAE), a mouse model of multiple sclerosis, when given orally to the hosts at 10 mg/kg daily beginning at the time of disease induction.

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